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/ Sunitinib Malate

苹果酸舒尼替尼 /Sunitinib Malate {[allProObj[0].p_purity_real_show]}

货号：A142950 同义名： 苹果酸苏尼替尼 / SU 11248 Malate;Sunitinib (malate)

Sunitinib Malate（SU 11248 Malate）是一种多靶点受体酪氨酸激酶抑制剂，对VEGFR2和PDGFRβ的IC50值分别为80 nM和2 nM。作为一种ATP竞争性抑制剂，马来酸舒尼替尼有效抑制Ire1α的自磷酸化及随后的RNase激活。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Sunitinib Malate 化学结构 CAS号：341031-54-7
Sunitinib Malate 化学结构
CAS号：341031-54-7
Sunitinib Malate 3D分子结构
CAS号：341031-54-7
Sunitinib Malate 化学结构 CAS号：341031-54-7
Sunitinib Malate 3D分子结构 CAS号：341031-54-7
规格 价格 会员价 库存 数量
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Sunitinib Malate 纯度/质量文件 产品仅供科研

货号：A142950 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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更多 >
产品名称 c-Kit ↓ 其他靶点 纯度
Tyrphostin AG1296 +

c-Kit (Swiss 3T3), IC50: 1.8 μM

 		PDGFR 99%+
Masitinib +

Kit, IC50: 200 nM

 		99%+
Motesanib Diphosphate +++

Kit, IC50: 8 nM

 		98%
Ki8751 ++

c-Kit, IC50: 40 nM

 		98+%
Tivozanib ++

c-Kit, IC50: 78 nM

 		99%+
Pazopanib +

c-Kit, IC50: 140 nM

 		99%
Sitravatinib +++

Kit, IC50: 6 nM

 		99%+
Pexidartinib +++

Kit, IC50: 10 nM

 		99%+
Lactate ++++

c-Kit, IC50: 2 nM

 		FLT3 85%
Amuvatinib +++

c-Kit (D816H), IC50: 10 nM

 		99%+
Imatinib Mesylate +

c-Kit, IC50: 100 nM

 		PDGFR 99%
AZD2932 +++

c-Kit, IC50: 9 nM

 		98%
Axitinib ++++

Kit, IC50: 1.7 nM

 		98%
Dovitinib ++++

c-Kit, IC50: 2 nM

 		FLT3 99%+
Sunitinib ✔ FLT3 98%
OSI-930 +

Kit, IC50: 80 nM

 		99%+
Telatinib ++++

c-Kit, IC50: 1 nM

 		99%+
Dasatinib monohydrate ++

c-Kit (wt), IC50: 79 nM

c-Kit (D816V), IC50: 37 nM

 		Src 98%
Dasatinib ++

c-Kit (wt), IC50: 79 nM

c-Kit (D816V), IC50: 37 nM

 		Src 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
产品名称 PDGFR ↓ PDGFRα ↓ PDGFRβ ↓ 其他靶点 纯度
Tyrphostin A9 +

PDGFR, IC50: 0.5 μM

 		EGFR 98%
Tyrphostin AG1296 99%+
Motesanib Diphosphate ++

PDGFR, IC50: 84 nM

 		98%
Pazopanib ++

PDGFR, IC50: 84 nM

 		99%
Imatinib +

PDGFR, IC50: 100 nM

 		c-Kit 98%
Imatinib Mesylate +

PDGFR, IC50: 100 nM

 		c-Kit 99%
Sennoside B ✔ 99%+
PP121 ++++

PDGFR, IC50: 2 nM

 		VEGFR,mTOR 99%+
Crenolanib ++++

PDGFRα, Kd: 2.1 nM

 		++++

PDGFRβ, Kd: 3.2 nM

 		99%+
Masitinib +

PDGFRα, IC50: 540 nM

 		+

PDGFRβ, IC50: 800 nM

 		99%+
Ki8751 ++

PDGFRα, IC50: 67 nM

 		c-Kit 98+%
Tivozanib ++

PDGFRα, IC50: 40 nM

 		++

PDGFRβ, IC50: 49 nM

 		99%+
Ponatinib ++++

PDGFRα, IC50: 1.1 nM

 		98%
Amuvatinib ++

PDGFRα (V561D), IC50: 40 nM

 		99%+
Axitinib +++

PDGFRα, IC50: 5.0 nM

 		++++

PDGFRβ, IC50: 1.6 nM

 		98%
CP-673451 +++

PDGFRα, IC50: 10 nM

 		++++

PDGFRβ, IC50: 1 nM

 		99%+
Telatinib +++

PDGFRα, IC50: 15 nM

 		c-Kit 99%+
Nintedanib ++

PDGFRα, IC50: 59 nM

 		++

PDGFRβ, IC50: 65 nM

 		99+%
Avapritinib ++++

PDGFRα (D842V), IC50: 0.5 nM

 		99%+
MK-2461 +++

PDGFRβ, IC50: 22 nM

 		98%+
Lactate +++

PDGFRβ, IC50: 27 nM

 		c-Kit,FLT3 85%
Linifanib ++

PDGFRβ, IC50: 66 nM

 		99%+
AZD2932 +++

PDGFRβ, IC50: 4 nM

 		c-Kit 98%
Dovitinib +++

PDGFRβ, IC50: 27 nM

 		c-Kit,FLT3 99%+
Sorafenib ++

PDGFRβ, IC50: 57 nM

mPDGFRβ, IC50: 57 nM

 		99%
Sunitinib ++++

PDGFRβ , IC50: 2 nM

 		FLT3 98%
Orantinib +++

PDGFRβ, Ki: 8 nM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
产品名称 VEGFR1 ↓ VEGFR2 ↓ VEGFR3 ↓ 其他靶点 纯度
Motesanib Diphosphate ++++

VEGFR1, IC50: 2 nM

 		++++

VEGFR2, IC50: 3 nM

VEGFR2/Flk1, IC50: 3 nM

 		+++

VEGFR3, IC50: 6 nM

 		RET,PDGFR 98%
Tivozanib ++

VEGFR1, IC50: 30 nM

 		+++

VEGFR2, IC50: 6.5 nM

 		++

VEGFR3, IC50: 15 nM

 		99%+
Brivanib +

VEGFR1, IC50: 380 nM

 		++

VEGFR2, IC50: 25 nM

Flk1, IC50: 25 nM

 		99%+
Regorafenib +++

VEGFR1, IC50: 13 nM

 		+++

VEGFR2, IC50: 4.2 nM

 		+

VEGFR3, IC50: 46 nM

 		RET 98%
Pazopanib +++

VEGFR1, IC50: 10 nM

 		++

VEGFR2, IC50: 30 nM

 		+

VEGFR3, IC50: 47 nM

 		c-Kit,FGFR,PDGFR 99%
Sitravatinib +++

VEGFR1 (FLT1), IC50: 6 nM

 		+++

VEGFR2 (KDR), IC50: 5 nM

 		++++

VEGFR3 (FLT4), IC50: 2 nM

 		99%+
Foretinib +++

VEGFR1/FLT1, IC50: 6.8 nM

 		++++

KDR, IC50: 0.86 nM

 		++++

VEGFR3/FLT4, IC50: 2.8 nM

 		Tie-2 99%+
MGCD-265 analog ++++

VEGFR1, IC50: 3 nM

 		++++

VEGFR2, IC50: 3 nM

 		++++

VEGFR3, IC50: 4 nM

 		Tie-2 99%+
Lactate +++

VEGFR1/FLT1, IC50: 10 nM

 		+++

VEGFR2/Flk1, IC50: 13 nM

 		+++

VEGFR3/FLT4, IC50: 8 nM

 		c-Kit,FLT3 85%
AEE788 +

FLT1, IC50: 59 nM

 		+

KDR, IC50: 77 nM

 		EGFR 98+%
Linifanib ++++

VEGFR1/FLT1, IC50: 3 nM

 		++++

VEGFR2/KDR, IC50: 4 nM

 		+

VEGFR3/FLT4, IC50: 190 nM

 		FLT3 99%+
Vatalanib 2HCl +

VEGFR1/FLT1, IC50: 77 nM

 		++

VEGFR2/KDR, IC50: 37 nM

VEGFR2/Flk1, IC50: 270 nM

 		+

VEGFR3/FLT4, IC50: 660 nM

 		c-Kit,c-Fms 99%+
Axitinib ++++

VEGFR1/FLT1, IC50: 0.1 nM

 		++++

VEGFR2/KDR, IC50: 0.2 nM

VEGFR2/Flk1, IC50: 0.18 nM

 		98%
Dovitinib +++

VEGFR1/FLT1, IC50: 10 nM

 		+++

VEGFR2/Flk1, IC50: 13 nM

 		+++

VEGFR3/FLT4, IC50: 8 nM

 		c-Kit,FLT3 99%+
ZM 306416 +

VEGFR1, IC50: 0.33 μM

 		Src 99%+
KRN-633 +

VEGFR1, IC50: 170 nM

 		+

VEGFR2, IC50: 160 nM

 		+

VEGFR3, IC50: 125 nM

 		c-Kit,BTK 98%
OSI-930 +++

FLT1, IC50: 8 nM

 		+++

KDR, IC50: 9 nM

 		99%+
Lenvatinib ++

VEGFR1/FLT1, IC50: 22 nM

 		++++

VEGFR2/KDR, IC50: 4.0 nM

 		+++

VEGFR3/FLT4, IC50: 5.2 nM

 		98%
NVP-BAW2881 +

hVEGFR1, IC50: 820 nM

 		+++

hVEGFR2, IC50: 9 nM

mVEGF2, IC50: 165 nM

 		+

hVEGFR3, IC50: 420 nM

 		98%
Cediranib +++

VEGFR1/FLT1, IC50: 5 nM

 		++++

VEGFR2/KDR, IC50: 0.5 nM

 		c-Kit 99%+
Nintedanib ++

VEGFR1, IC50: 34 nM

 		+++

VEGFR2, IC50: 13 nM

 		+++

VEGFR3, IC50: 13 nM

 		FLT3 99+%
BMS-794833 ++

VEGFR2, IC50: 15 nM

 		99%+
SKLB1002 ++

VEGFR2, IC50: 32 nM

 		98%
Cabozantinib S-malate ++++

VEGFR2/KDR, IC50: 0.035 nM

 		99+%
Ki8751 ++++

VEGFR2, IC50: 0.9 nM

 		c-Kit 98+%
SU 5402 ++

VEGFR2, IC50: 20 nM

 		98%
Rivoceranib Mesylate ++++

VEGFR2, IC50: 1 nM

 		RET 98+%
Ponatinib ++++

VEGFR2, IC50: 1.5 nM

 		98%
LY2874455 +++

VEGFR2, IC50: 7 nM

 		99%+
ZM323881 HCl ++++

VEGFR2, IC50: <2 nM

 		98%
AZD2932 +++

VEGFR-2, IC50: 8 nM

 		c-Kit 98%
Cabozantinib ++++

VEGFR2/KDR, IC50: 0.035 nM

 		98%
Sorafenib ++

VEGFR2, IC50: 90 nM

VEGFR2/Flk1, IC50: 90 nM

 		99%
CYC-116 ++

VEGFR2, Ki: 44 nM

 		FLT3 99%+
Golvatinib ++

VEGFR2, IC50: 16 nM

 		99%+
Sunitinib +

VEGFR2 , IC50: 80 nM

 		FLT3 98%
RAF265 ++

VEGFR2, EC50: 30 nM

 		99%+
PD173074 99%+
BFH772 ++++

VEGFR2, IC50: 3 nM

 		98%
Semaxinib +

VEGFR2/Flk1, IC50: 1.23 μM

 		98%
Vandetanib ++

VEGFR2, IC50: 40 nM

 		+

VEGFR3, IC50: 110 nM

 		EGFR 98%
SAR131675 ++

VEGFR3, IC50: 23 nM

 		99%+
ENMD-2076 +

VEGFR2/KDR, IC50: 58.2 nM

 		++

VEGFR3/FLT4, IC50: 15.9 nM

 		RET,FLT3 98%
Telatinib +++

VEGFR2, IC50: 6 nM

 		++++

VEGFR3, IC50: 4 nM

 		c-Kit 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Sunitinib Malate 生物活性

描述 VEGFR (vascular endothelial growth factor) and PDGFR (platelet-derived growth factor receptor) are critical roles in tumor growth and suvival via autocrine and paracrine loops, making them the well validated targets for the treatment of cancers. Sunitinib Malate is the Malate form of Sunitinib. Sunitinib is a multiple RTKs inhibitor with IC50 values of 2nM and 80nM for VEGFR2 and PDGFRβ (measured by kinase activity)[1], respectively, also shows inhibition against KIT and FLT3 receptor[2]. The cellular kinase activity induced by VEGF/PDGF can be inhibited by Sunitinib with IC50 value of 5-50nM/10nM in 3T3 cells, while the PDGF-induced cell growth can be inhibited by Sunitinib with IC50 of 8nM[1]. Daily oral administration of Sunitinib at dose of 80mg/kg reduced growth of established SF763T tumor xenografts in athymic mice, as well as suppressed Colo205 tumor growth. Consistent with the cellular kinase study, the inhibition by Sunitinib against p-PDGFRβ can be observed in tumor after a single dose at 80mg/kg in mice bearing SF767T tumors and mice bearing Colo205 tumors, as well as suppressed p-FLK1 in A375 xenograft mice dosed 40mg/kg Sunitinib[2].
作用机制 Sunitinib is an ATP-competitive multitargeted tyrosine kinase inhibitor.[3]

Sunitinib Malate 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
3T3 Kinase Assay Inhibition of PDGF-induced BrdU incorporation with IC50 of 0.007 μM 12646019
3T3 Growth Inhibition Assay Inhibition of Platelet-derived growth factor induced 3T3 cell proliferation with IC50 of 0.01 μM 12646019
3T3 Function Assay Inhibition of Vascular endothelial growth factor receptor with IC50 of 0.05 μM 12646019
3T3 Kinase Assay 20 min Cellular inhibition of VEGF induced human KDR phosphorylation with IC50 of 0.022 μM 16162008

Sunitinib Malate 动物研究

Dose Rat: 0.5 mg/kg[5] (p.o.), 1 mg/kg - 10 mg/kg[6] (p.o.) Mice: 40 mg/kg[7] (p.o.)
Administration p.o.
Pharmacokinetics
Animal Rats[8]
Dose 2 mg/kg (i.v. or p.o.)
Administration i.v.
p.o.
F 112 ± 34% (p.o.)
T1/2 2.52 ± 0.04 h (i.v.)
AUCtlast 896 ± 461 ng·h/ml (p.o.)
Tmax 2.0 ± 2.0 h (p.o.)
Cmax 177 ± 86 ng/ml (p.o.)
AUC0→∞ 996 ± 439 ng·h/ml (i.v.)
1178 ± 691 ng·h/ml (p.o.)
CLs 40 ± 23 ml/min/kg (i.v.)

Sunitinib Malate 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00663559 Carcinoma Renal Cells Phase 2 Completed - Spain ... 展开 >> Hospital Central de Asturias Oviedo, Asturias, Spain, 33006 Hospital Parc Taulí Sabadell, Barcelona, Spain, 08208 Hospital CLINIC Barcelona, Spain, 08036 Hospital Reina Sofía Córdoba, Spain, 14004 Hospital de Jaén Jaén, Spain, 23007 Hospital Clínico San Carlos Madrid, Spain, 28040 Hospital lozano Blesa Zaragoza, Spain, 50009 收起 <<
NCT03097601 - Active, not recruiting December 30, 2019 France ... 展开 >> Centre Antoine LACASSAGNE Nice, France, 06189 收起 <<
NCT01243359 Clear Cell Renal Cell Carcinom... 展开 >>a Recurrent Renal Cell Cancer Stage I Renal Cell Cancer Stage II Renal Cell Cancer Stage III Renal Cell Cancer Stage IV Renal Cell Cancer Unspecified Adult Solid Tumor, Protocol Specific 收起 << Phase 1 Completed - United States, Maryland ... 展开 >> Johns Hopkins University/Sidney Kimmel Cancer Center Baltimore, Maryland, United States, 21287 United States, Wisconsin University of Wisconsin Hospital and Clinics Madison, Wisconsin, United States, 53792 收起 <<

Sunitinib Malate 参考文献

[1]Shukla S, Robey RW, et al. Sunitinib (Sutent, SU11248), a small-molecule receptor tyrosine kinase inhibitor, blocks function of the ATP-binding cassette (ABC) transporters P-glycoprotein (ABCB1) and ABCG2. Drug Metab Dispos. 2009 Feb;37(2):359-65.

[2]Sun L, Liang C, et al. Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl] -2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase. J Med Chem. 2003 Mar 27;46(7):1116-9.

[3]Mendel DB, Laird AD, et al. In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin Cancer Res. 2003 Jan;9(1):327-37.

[4]Zhou Q, Gallo JM. Differential effect of sunitinib on the distribution of temozolomide in an orthotopic glioma model. Neuro Oncol. 2009;11(3):301-10.

[5]sunitinib malate

[6]Blasi E, Heyen J, et al. Sunitinib, a receptor tyrosine kinase inhibitor, increases blood pressure in rats without associated changes in cardiac structure and function. Cardiovasc Ther. 2012 Oct;30(5):287-94.

[7]Gotink KJ, Broxterman HJ, et al. Acquired tumor cell resistance to sunitinib causes resistance in a HT-29 human colon cancer xenograft mouse model without affecting sunitinib biodistribution or the tumor microvasculature. Oncoscience. 2014 Dec 15;1(12):844-53. eCollection 2014.

[8]Sutent

Sunitinib Malate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.88mL

0.38mL

0.19mL

9.39mL

1.88mL

0.94mL

18.78mL

3.76mL

1.88mL

Sunitinib Malate 技术信息

CAS号341031-54-7
分子式C26H33FN4O7
分子量 532.561
别名 苹果酸苏尼替尼 ;SU 11248 Malate;Sunitinib (malate);SU11248
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C
溶解度

DMSO: 14 mg/mL(26.29 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 12 mg/mL(22.53 mM)，配合低频超声，并调节pH至3
动物实验配方

PO 0.5% CMC-Na 47 mg/mL suspension

Tags: Sunitinib Malate | SU 11248 Malate;Sunitinib (malate);SU11248 | 苹果酸苏尼替尼 | VEGFR | PDGFR | c-Kit | AmBeed-信号通路专用抑制剂 | Sunitinib Malate 纯度/质量文件 | Sunitinib Malate 亚型比较 | Sunitinib Malate 生物活性 | Sunitinib Malate 细胞研究 | Sunitinib Malate 动物研究 | Sunitinib Malate 临床数据 | Sunitinib Malate 参考文献 | Sunitinib Malate 实验方案 | Sunitinib Malate 技术信息

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